Alfentanil

CLINICAL USE


Opioid analgesic:

  • Short surgical procedures
  • Intensive care sedation

    DOSE IN NORMAL RENAL FUNCTION

  • IV injection:

    Spontaneous respiration: up to


    500 micrograms over 30 seconds;
    supplemental dose: 250 micrograms
    assisted ventilation: 30–50


    micrograms/kg; supplemental dose:
    15 micrograms/kg

  • By IV infusion with assisted ventilation:

    loading dose 50–100 micrograms/kg as
    bolus or fast infusion over 10 minutes,
    followed by 0.5–1 micrograms/kg/minute.
    Discontinue infusion 30 minutes before
    anticipated end of surgery

  • For analgesia and suppression of

    respiratory activity during intensive care
    with assisted ventilation: by IV infusion
    2 mg/hour, adjusted according to response
    (usual range 0.5–10 mg/hour)

  • For more rapid initial control give 5 mg

    IV in divided portions over 10 minutes
    (slower if hypotension or bradycardia
    develops); additional doses of 0.5–1 mg
    may be given by IV injection during short
    painful procedures

    PHARMACOKINETICS


  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    453 (as hydrochloride)
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    92
  • %Excreted unchanged in urine &nbsp &nbsp :
    0.4
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :
    0.4–1
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :
    1–2 (average
    90 minutes)/
    Unchanged

    DOSE IN RENAL IMPAIRMENT


    GFR (mL/MIN)


  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function
  • 10 to 20 &nbsp &nbsp : Dose as in normal renal function
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp :
    Dose as in normal renal function

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES


  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:
    Not dialysed. Dose as in normal renal function

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    Not dialysed. Dose as in normal renal function
  • HDF/high flux &nbsp :
    Unknown dialysability. Dose as in
    normal renal function
  • CAV/VVHD &nbsp &nbsp &nbsp:
    Not dialysed. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS


    Potentially hazardous interactions with other drugs

  • Antidepressants: possible CNS excitation

    or depression (hypertension or
    hypotension) in patients also receiving
    MAOIs (including moclobemide) – avoid
    concomitant use; possibly increased
    sedative effects with tricyclics

  • Antifungals: metabolism inhibited by

    fluconazole and ketoconazole (risk
    of prolonged or delayed respiratory
    depression); metabolism possibly inhibited
    by itraconazole

  • Antivirals: concentration possibly

    increased by ritonavir

  • Sodium oxybate: enhanced effect of

    sodium oxybate – avoid concomitant use

    ADMINISTRATION


    Reconstition



    Route


    IV bolus,

    IV infusion

    Rate of Administration


    See dose

    Comments

  • Alfentanil can be mixed with sodium

    chloride 0.9%, glucose 5%, or compound
    sodium lactate injection (Hartmann’s
    solution) at a concentration of 0.5 mg/
    mL, but can be used at 2 mg/mL or even
    undiluted at 5 mg/mL.

    OTHER INFORMATION

  • Free fraction of drug is increased in renal

    failure, hence dose requirements may be
    reduced

  • IV administration: 500 micrograms

    alfentanil has peak effect in 90 seconds,
    and provides analgesia for 5–10 minutes
    (in unpremedicated adults)

  • Transient fall in BP and bradycardia may

    occur on administration

  • Analgesic potency = ¼ that of fentanyl

    Duration of action = ⅓ that of an equi-

    analgesic dose of fentanyl

  • Onset of action = 4 times more rapid than

    an equi-analgesic dose of fentanyl